ATE197043T1 - Pyrimidinyl-essigsäureamide als elastase inhibitoren - Google Patents

Pyrimidinyl-essigsäureamide als elastase inhibitoren

Info

Publication number
ATE197043T1
ATE197043T1 AT92307389T AT92307389T ATE197043T1 AT E197043 T1 ATE197043 T1 AT E197043T1 AT 92307389 T AT92307389 T AT 92307389T AT 92307389 T AT92307389 T AT 92307389T AT E197043 T1 ATE197043 T1 AT E197043T1
Authority
AT
Austria
Prior art keywords
substituted heterocycles
pyrimidinyl
acid amides
elastase inhibitors
hle
Prior art date
Application number
AT92307389T
Other languages
English (en)
Inventor
Peter Robert Bernstein
Philip Duke Edwards
Andrew Shaw
Royston Martin Thomas
Chris Allan Veale
Peter Warner
Donald John Wolanin
Original Assignee
Zeneca Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB919117641A external-priority patent/GB9117641D0/en
Priority claimed from GB929208378A external-priority patent/GB9208378D0/en
Priority claimed from GB929214447A external-priority patent/GB9214447D0/en
Application filed by Zeneca Ltd filed Critical Zeneca Ltd
Application granted granted Critical
Publication of ATE197043T1 publication Critical patent/ATE197043T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C07D239/36—One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Separation Using Semi-Permeable Membranes (AREA)
  • Compositions Of Oxide Ceramics (AREA)
  • Nonmetallic Welding Materials (AREA)
AT92307389T 1991-08-15 1992-08-12 Pyrimidinyl-essigsäureamide als elastase inhibitoren ATE197043T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB919117641A GB9117641D0 (en) 1991-08-15 1991-08-15 Substituted heterocycles
GB929208378A GB9208378D0 (en) 1992-04-16 1992-04-16 Substituted heterocycles
GB929214447A GB9214447D0 (en) 1992-07-08 1992-07-08 Substituted heterocycles

Publications (1)

Publication Number Publication Date
ATE197043T1 true ATE197043T1 (de) 2000-11-15

Family

ID=27265822

Family Applications (1)

Application Number Title Priority Date Filing Date
AT92307389T ATE197043T1 (de) 1991-08-15 1992-08-12 Pyrimidinyl-essigsäureamide als elastase inhibitoren

Country Status (16)

Country Link
US (1) US5254558A (de)
EP (1) EP0528633B1 (de)
JP (1) JPH05286946A (de)
KR (1) KR930004276A (de)
AT (1) ATE197043T1 (de)
CA (1) CA2076226C (de)
CZ (1) CZ251792A3 (de)
DE (1) DE69231513T2 (de)
FI (1) FI923661A7 (de)
GB (1) GB9216272D0 (de)
HU (1) HUT61732A (de)
IE (1) IE922586A1 (de)
IL (1) IL102805A0 (de)
NO (1) NO923197L (de)
NZ (1) NZ243950A (de)
ZW (1) ZW13292A1 (de)

Families Citing this family (51)

* Cited by examiner, † Cited by third party
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US5521179A (en) * 1991-04-18 1996-05-28 Zeneca Limited Heterocyclic amides
US5441960A (en) * 1992-04-16 1995-08-15 Zeneca Limited 1-pyrimidinylacetamide human leukocyte elastate inhibitors
DE69314169T2 (de) * 1992-04-16 1998-01-15 Zeneca Ltd Peptide mit eine alphaaminoboronaire gruppe and ihre verwendung als elastasehemmer
US5486529A (en) * 1992-04-16 1996-01-23 Zeneca Limited Certain pyridyl ketones for treating diseases involving leukocyte elastase
GB9211783D0 (en) * 1992-06-04 1992-07-15 Ici Plc Amide derivatives
GB9214053D0 (en) * 1992-07-02 1992-08-12 Ici Plc Heterocyclic amides
US6100238A (en) * 1994-11-21 2000-08-08 Cortech Inc. Indole and tetrahydroisoquinoline containing Alpha-keto oxadiazoles as serine protease inhibitors
US5618792A (en) * 1994-11-21 1997-04-08 Cortech, Inc. Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase
US6001814A (en) * 1994-11-21 1999-12-14 Cortech Inc. Serine protease inhibitors
US5998379A (en) * 1994-11-21 1999-12-07 Cortech Inc. Serine protease inhibitors-proline analogs
US6150334A (en) * 1994-11-21 2000-11-21 Cortech, Inc. Serine protease inhibitors-tripeptoid analogs
US6015791A (en) * 1994-11-21 2000-01-18 Cortech Inc. Serine protease inhibitors-cycloheptane derivatives
US6159938A (en) * 1994-11-21 2000-12-12 Cortech, Inc. Serine protease inhibitors comprising α-keto heterocycles
US6001811A (en) * 1994-11-21 1999-12-14 Cortech Inc. Serine protease inhibitors--N-substituted derivatives
US20020119985A1 (en) 1994-11-21 2002-08-29 Albert Gyorkos Serine protease inhibitors
US6001813A (en) * 1994-11-21 1999-12-14 Cortech Inc. Val-pro containing α-keto oxadiazoles as serine protease inhibitors
US5658930A (en) * 1994-12-13 1997-08-19 Corvas International, Inc. Aromatic heterocyclic derivatives as enzyme inhibitors
US5656645A (en) * 1994-12-13 1997-08-12 Corvas International, Inc. Aromatic heterocyclic derivatives as enzyme inhibitors
CN1188401C (zh) * 1995-04-27 2005-02-09 三菱制药株式会社 杂环类酰胺化合物及其医药用途
BR9712000A (pt) 1996-09-06 1999-08-24 Nippon Kayaku Kk Derivados de acetamida sais dos mesmos composi-Æo farmac-utica inibidores de protease de quimase de desgranula-Æo de mastÄcitos ou de libera-Æo de histamina de mastÄcitos e de ativa-Æo de eosinÄfilo ou de libera-Æo de oxig-nio ativo de eosinÄfilo e processo para produzir os dervados de acetamida
US6080738A (en) * 1996-10-25 2000-06-27 Yoshitomi Pharmaceuticals Industries, Ltd. Heterocyclic amide compounds and medicinal uses thereof
TR199901681T2 (xx) * 1996-12-06 2000-03-21 Cortech, Inc. Serin proteas inhibit�rleri.
US6656910B2 (en) 1997-12-04 2003-12-02 Cortech, Inc. Serine protease inhibitors
WO1999041277A1 (en) 1998-02-17 1999-08-19 Nippon Kayaku Kabushiki Kaisha Novel acetamide derivative and use thereof
CN1160075C (zh) 1998-03-11 2004-08-04 卫福有限公司 杂环酰胺化合物在制备IgE抗体产生抑制剂中的用途
US6255453B1 (en) 1998-06-03 2001-07-03 Cortech, Inc. Peptoid and nonpeptoid containing alpha-keto oxadiazoles as serine protease inhibitors
KR20020011970A (ko) * 1999-03-12 2002-02-09 우에노 도시오 피리미딘 유도체 및 그 제조 방법
US7015230B1 (en) 1999-05-19 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6664255B1 (en) 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
US6716838B1 (en) 1999-05-19 2004-04-06 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
US6750342B1 (en) 1999-05-19 2004-06-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6458952B1 (en) 1999-05-19 2002-10-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6653316B1 (en) 1999-05-19 2003-11-25 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6867217B1 (en) 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
CA2375229A1 (en) * 1999-06-17 2000-12-28 Source Precision Medicine, Inc. Method and compounds for inhibiting activity of serine elastases
WO2001023361A1 (en) * 1999-09-27 2001-04-05 Ono Pharmaceutical Co., Ltd. Pyrimidine derivatives, process for preparing the derivatives and drugs containing the same as the active ingredient
WO2001068605A1 (en) 2000-03-13 2001-09-20 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
ATE289299T1 (de) 2000-04-05 2005-03-15 Pharmacia Corp Polyzyclisch aryl und heteroaryl substituierte 4- pyronen verwendbar als selektive hemmung von dem koagulationsprozess
AU2001251315A1 (en) 2000-04-05 2001-10-23 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade
EP1274676A2 (de) 2000-04-17 2003-01-15 Pharmacia Corporation Polycyclische aryl- und heteroaryl- substuierte 1,4-chinone zur selektiven hemmung des blutgerinnungsprozesses
WO2001087851A1 (en) * 2000-05-18 2001-11-22 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
CA2416248A1 (en) * 2000-07-18 2002-01-24 Neurogen Corporation 5-substituted 2-aryl-4-pyrimidinones
US7015223B1 (en) 2000-11-20 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl 1,2,4-triazinones useful for selective inhibition of the coagulation cascade
CA2430037A1 (en) 2000-11-20 2002-05-30 Michael S. South Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade
US7119094B1 (en) 2000-11-20 2006-10-10 Warner-Lambert Company Substituted polycyclic aryl and heteroarpyl pyrazinones useful for selective inhibition of the coagulation cascade
HUP0303631A2 (hu) * 2000-12-26 2004-03-01 Ono Pharmaceutical Co., Ltd. Pirimidinszármazékok és eljárás előállításukra
MXPA04003170A (es) 2001-10-03 2004-07-08 Pharmacia Corp Compuestos policiclicos, sustituidos, provisto de 5 miembros, utiles para la inhibicion selectiva de la cascada de coagulacion.
BR0213092A (pt) 2001-10-03 2004-10-19 Pharmacia Corp Compostos heterocìclicos de 6 elementos úteis para a inibição seletiva da cascata de coagulação
MXPA05002644A (es) * 2002-09-10 2005-09-20 Bayer Healthcare Ag Derivados de pirimidinona como agentes terapeuticos contra procesos de remodelacion, isquemicos e inflamatorios agudos y cronicos.
TW200500341A (en) * 2002-11-12 2005-01-01 Astrazeneca Ab Novel compounds
PE20050159A1 (es) 2003-05-27 2005-04-19 Vertex Pharma Derivados de acido 3-[2-(3-amino-2-oxo-2h-piridin-1-il)-acetilamino]-4-oxo-pentanoico como inhibidores de caspasa

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GB8600263D0 (en) * 1985-01-22 1986-02-12 Ici America Inc Peptide derivatives

Also Published As

Publication number Publication date
HUT61732A (en) 1993-03-01
FI923661A7 (fi) 1993-02-16
NO923197L (no) 1993-02-16
DE69231513T2 (de) 2001-03-01
DE69231513D1 (de) 2000-11-23
EP0528633B1 (de) 2000-10-18
US5254558A (en) 1993-10-19
IL102805A0 (en) 1993-01-31
EP0528633A1 (de) 1993-02-24
CA2076226A1 (en) 1993-02-16
CZ251792A3 (en) 1993-02-17
HU9202640D0 (en) 1992-10-28
KR930004276A (ko) 1993-03-22
ZW13292A1 (en) 1993-05-05
CA2076226C (en) 2004-09-21
FI923661A0 (fi) 1992-08-14
NZ243950A (en) 1995-05-26
JPH05286946A (ja) 1993-11-02
IE922586A1 (en) 1993-02-24
NO923197D0 (no) 1992-08-14
GB9216272D0 (en) 1992-09-09

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